HUP0204262A2 - Benzogyűrűvel kondenzált heterociklusos csoportot tartalmazó nikotinamid-származékok, továbbá e vegyületeket tartalmazó, a PDE4 izozimek szelektív gátlására adható gyógyászati készítmények - Google Patents

Benzogyűrűvel kondenzált heterociklusos csoportot tartalmazó nikotinamid-származékok, továbbá e vegyületeket tartalmazó, a PDE4 izozimek szelektív gátlására adható gyógyászati készítmények

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HUP0204262A2
HUP0204262A2 HU0204262A HUP0204262A HUP0204262A2 HU P0204262 A2 HUP0204262 A2 HU P0204262A2 HU 0204262 A HU0204262 A HU 0204262A HU P0204262 A HUP0204262 A HU P0204262A HU P0204262 A2 HUP0204262 A2 HU P0204262A2
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nr15r12
group
nr14c
phenyl
cycloalkyl
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HU0204262A
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Robert James Chamber
Anthony Marfat
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Pfizer Products Inc.
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Publication of HUP0204262A2 publication Critical patent/HUP0204262A2/hu

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Abstract

A találmány tárgyát az (1.0.0) általános képletű vegyületek, valamintezeket tartalmazó gyógyászati készítmények képezik. A találmányszerinti (1.0.0) általános képletű vegyületek eredményesen adhatókgyulladásos betegségek, asztma, reumás arthritis, bronchitis,psoriasis, autoimmun/gyulladásos betegségek és hasonlók kezelésére. Az(1.0.0) általános képletben a szubsztituensek jelentése igen sokféle,így például - m értéke 0, 1 vagy 2; - n értéke 1 vagy 2; - W jelentése-O-, -S(=O)t-, ahol t értéke 0, 1 vagy 2; vagy -N(R3)-, ahol R3jelentése az alábbiakban megadottal azonos; - Y jelentése =C(RE)- vagy-N[<(O)]-; - ahol - - RE jelentése például -H, -F, -Cl, -CN, -NO2, 1-4szénatomos alkil-, 1-3 szénatomos alkoxi-, -OH vagy -C(=O)NR12R13,ahol R12 és R13 jelentése az alábbiakban megadottal azonos; - RA és RBjelentése egymástól függetlenül például -CF3, 1-6 szénatomos alkil-,3-7 szénatomos cikloalkil-, fenil-, benzil- vagy heterociklusoscsoport; ahol a fentiekben említett alkil-, cikloalkil-, fenil-,benzil- vagy heterociklusos csoportok mindegyike egymástól függetlenül0-3 szubsztituenst hordozhat; - Q jelentése például fenil-, pirrolil-,furanil-, tienil-, piridil-, pirimidinil-, imidazolil-, tiazolil-,oxazolil-, monociklusos-(5-7 szénatomos cikloalkil)-csoport, vagybiciklusos-(7-10 szénatomos cikloalkil)- vagy 7-10 szénatomoscikloalkenilcsoport, előnyösen norbornanil- vagy norbornenil-csoport;R1 és R2 jelentése például -Cl, -R12, -OR12, -S(=O)pR12, -C(=O)OR12, -OC(=O)R12, -CN; -NO2, -C(=O)NR12R13, -OC(=O)NR12R13; -NR14C(=O)NR15R12, -NR14C(=NR14)NR15R12, -NR14C(=NCN)NR15R12, -OC(=N-NO2)NR15R12 -NR15R12; -CH2NR15R12, -NR14C(=O)R12; - R3 jelentésepéldául 1-3 szénatomos alkil-, 1-3 szénatomos alkoxi-, -OH-, fenil-vagy benzilcsoport, - R4 jelentése egymástól függetlenül például - (a)2-4 szénatomos alkinil-, -R12, -OR12, -S(=O)pR12, -C(=O)OR12, -OC(=O)R12, -CN, -NO2, -C(=O)NR15R12. - R5 és R6 jelentése együttesenrészlegesen telített öttagú heterociklusos gyűrűt alkot, amelyheteroatomként nitrogénatomot és/vagy oxigénatomot vagy kénatomottartalmaz; - Z jelentése egymástól függetlenül -OR12, -C(=O)R12 vagy -CN képletű csoport, ahol R12 jelentése a fentiekben megadottal azonos. Ó
HU0204262A 2000-01-31 2001-01-30 Benzogyűrűvel kondenzált heterociklusos csoportot tartalmazó nikotinamid-származékok, továbbá e vegyületeket tartalmazó, a PDE4 izozimek szelektív gátlására adható gyógyászati készítmények HUP0204262A2 (hu)

Applications Claiming Priority (2)

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US17928400P 2000-01-31 2000-01-31
PCT/IB2001/000124 WO2001057036A1 (en) 2000-01-31 2001-01-30 Nicotinamide benzofused-heterocyclyl derivatives useful as selective inhibitors of pde4 isozymes

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HUP0204262A2 true HUP0204262A2 (hu) 2003-04-28

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